173901-90-1Relevant articles and documents
Potent, elective human beta3 adrenergic receptor agonists containing a substituted indoline-5-sulfonamide pharmacophore.
Mathvink,Barritta,Candelore,Cascieri,Deng,Tota,Strader,Wyvratt,Fisher,Weber
, p. 1869 - 1874 (1999)
A series of compounds possessing an N-substituted indoline-5-sulfonamide pharmacophore was prepared and evaluated for their human beta3 adrenergic receptor agonist activity. The SAR of a wide range of urea and heterocyclic substituents is discussed. 4-Octyl thiazole compound 8c was the most potent and selective compound in the series, with 2800-fold selectivity over beta1 binding and 1400-fold selectivity over beta2 binding.
SUBSTITUTED SULFONAMIDES AS SELECTIVE BETA3 AGONISTS FOR THE TREATMENT OF DIABETES AND OBESITY
-
, (2008/06/13)
Substituted sulfonamides are selective β 3 adrenergic receptor agonists with very little β 1 and β 2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent